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    • 4. 发明申请
    • STABLE NON-ALCOHOLIC FOAMABLE PHARMACEUTICAL EMULSION COMPOSITIONS WITH AN UNCTUOUS EMOLLIENT AND THEIR USES
    • 稳定的非醇性可发泡医药乳胶组合物及其使用方法及其用途
    • WO2009007785A2
    • 2009-01-15
    • PCT/IB2007/004683
    • 2007-11-14
    • FOAMIX LTD.BERMAN, TalTAMARKIN, DovEINI, MeirFRIEDMAN, DoronSCHUZ, David
    • BERMAN, TalTAMARKIN, DovEINI, MeirFRIEDMAN, DoronSCHUZ, David
    • A61K9/12
    • A61K9/0014A61K8/046A61K8/39A61K8/731A61K8/86A61K9/1075A61K9/122A61Q7/00A61Q19/00
    • A stable non-alcoholic foamable pharmaceutical emulsion composition includes an unctuous emollient, at a concentration of about 0.5% to about 49% by weight; at least one multi-active agent; at a concentration of about 0.5% to about 15% by weight; water; an effective amount of an active pharmaceutical agent having a degree of solubility in the emulsion composition; and at least one liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the unctuous emollient comprises a petrolatum alone or in combination with other unctuous agents; wherein the multi active agent is selected from the group consisting of (a) two or more complex emulgators wherein there is a difference of about 4 or more units between the HLB values of two of the emulgators or there is a significant difference in the chemical nature or structure of two of the emulgators; (b) a surfactant and a foam adjuvant or co surfactant, wherein the surfactant has a HLB close to the required HLB of the oil phase; (c) a surfactant and a liquid wax, wherein the surfactant has a HLB close to the required HLB of the oil phase; (d) a surfactant and a polymeric agent other than starch or a modified starch ester, wherein the surfactant has a HLB close to the required HLB of the oil phase; (e) a polymeric agent and a foam adjuvant or co surfactant, which can cooperate to stabilize the emulsion; (f) a single surfactant without a long polymeric side chain that is composed of a mixture of esters having a HLB close to the required HLB of the oil phase; combinations of any of the above, and wherein the composition is substantially flowable is stored in an pressurized container and upon release expands to form a breakable foam.
    • 稳定的不含酒精的可发泡药物乳剂组合物包含浓度为约0.5重量%至约49重量%的润滑剂; 至少一种多活性剂; 浓度为约0.5重量%至约15重量% 水; 有效量的在乳剂组合物中具有溶解度的活性药剂; 和至少一种液体或压缩气体推进剂,其浓度为全部组合物的约3重量%至约25重量% 其中所述润滑剂单独包含凡士林或与其他油性剂组合; 其中所述多活性剂选自(a)两种或更多种复合乳化剂,其中两种乳化剂的HLB值之间存在约4个或更多单元的差异,或者在化学性质上存在显着差异 或两个乳化器的结构; (b)表面活性剂和泡沫辅助剂或助表面活性剂,其中表面活性剂的HLB接近油相所需的HLB; (c)表面活性剂和液体蜡,其中表面活性剂的HLB接近油相所需的HLB; (d)除淀粉或改性淀粉酯以外的表面活性剂和聚合剂,其中表面活性剂的HLB接近油相所需的HLB; (e)聚合物试剂和泡沫辅助剂或共表面活性剂,其可协作以稳定乳液; (f)不含长聚合物侧链的单一表面活性剂,其由HLB接近油相所需HLB的酯的混合物组成; 上述任一种的组合,并且其中组合物基本可流动,将其储存在加压容器中,并在释放时膨胀形成易碎泡沫。
    • 5. 发明申请
    • FOAMABLE COMPOSITIONS AND KITS COMPRISING ONE OR MORE OF A CHANNEL AGENT, A CHOLINERGIC AGENT, A NITRIC OXIDE DONOR, AND RELATED AGENTS AND THEIR USES
    • 包含一个或多个通道代理,化学试剂,氮氧化物和相关试剂及其用途的可燃组合物和试剂盒
    • WO2008110872A2
    • 2008-09-18
    • PCT/IB2007/004522
    • 2007-06-22
    • FOAMIX LTD.TAMARKIN, DovEINI, MeirFRIEDMAN, DoronBERMAN, TalBESONOV, Alex
    • TAMARKIN, DovEINI, MeirFRIEDMAN, DoronBERMAN, TalBESONOV, Alex
    • A61K9/00A61K9/12A61K31/506A61K31/44A61K31/55
    • A61K9/0014A61K9/122A61K9/1274A61K31/44A61K31/506A61K31/55A61K47/12A61K47/26A61K47/34A61K47/38
    • The present invention relates to a foamable therapeutic composition comprising: (a) a therapeutically effective concentration of at least one active agent selected from the group consisting of a channel agent, a cholinergic agent, and a nitric oxide donor; and (b) a foamable carrier comprising: i. about 50% to about 98% of a solvent selected from the group consisting of water; a hydrophilic solvent; a hydrophobic solvent; a potent solvent; a polar solvent, a silicone, an emollient, and mixtures thereof; ii. 0% to about 48% of a secondary solvent selected from the group consisting of water; a hydrophilic solvent; a hydrophobic solvent; a potent solvent; a polar solvent, a silicone, an emollient, a co-solvent, a penetration enhancer and mixtures thereof; iii. a surface-active agent; iv. about 0% to about 5% by weight of at least one polymeric agent; and v. a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the composition is housed in a container and is substantially flowable, and which upon release expands to form a breakable foam; and wherein the foamable carrier is selected to generate a foam of good to excellent quality. The invention further provides a method of treating, alleviating or preventing a disorder of mammalian subject, comprising administering such a composition to an afflicted target site.
    • 本发明涉及可发泡治疗组合物,其包含:(a)治疗有效浓度的至少一种选自通道剂,胆碱能药和一氧化氮供体的活性剂; 和(b)可发泡载体,包括:i。 约50%至约98%的选自水的溶剂; 亲水性溶剂; 疏水溶剂; 有效溶剂; 极性溶剂,硅氧烷,软化剂及其混合物; II。 0%至约48%的选自水的第二溶剂; 亲水性溶剂; 疏水溶剂; 有效溶剂; 极性溶剂,硅氧烷,软化剂,​​助溶剂,渗透增强剂及其混合物; III。 表面活性剂; IV。 约0重量%至约5重量%的至少一种聚合物; 和v。浓度为总组合物重量的约3%至约25%的液化或压缩气体推进剂; 其中所述组合物容纳在容器中并且基本上是可流动的,并且其在释放时膨胀以形成可破坏的泡沫; 并且其中所述可发泡载体被选择以产生良好至优异质量的泡沫。 本发明进一步提供治疗,减轻或预防哺乳动物受试者病症的方法,包括将所述组合物施用于受影响的靶位点。